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Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.

Abstract PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq ~ 12.5??g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 ?g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.
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Authors

Mayor MeshTerms

Micelles

Keywords
Journal Title pharmaceutical development and technology
Publication Year Start
%A Adams, Monica L.; Rao, Venkatramana M.; Thakur, Ajit; Hussain, Munir A.
%T Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.
%J Pharmaceutical development and technology, vol. 15, no. 3, pp. 266-275
%D 06/2010
%V 15
%N 3
%M eng
%B PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq ~ 12.5??g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 ?g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.
%K Carboxylic Acids, Chemistry, Pharmaceutical, Colloids, Hydrogen-Ion Concentration, Micelles, Polyethylene Glycols, Polymers, Solubility, Surface-Active Agents, X-Ray Diffraction
%P 266
%L 275
%Y 10.3109/10837450903170772
%W PHY
%G AUTHOR
%R 2010.......15..266A

@Article{Adams2010,
author="Adams, Monica L.
and Rao, Venkatramana M.
and Thakur, Ajit
and Hussain, Munir A.",
title="Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.",
journal="Pharmaceutical development and technology",
year="2010",
month="Jun",
volume="15",
number="3",
pages="266--275",
keywords="Carboxylic Acids",
keywords="Chemistry, Pharmaceutical",
keywords="Colloids",
keywords="Hydrogen-Ion Concentration",
keywords="Micelles",
keywords="Polyethylene Glycols",
keywords="Polymers",
keywords="Solubility",
keywords="Surface-Active Agents",
keywords="X-Ray Diffraction",
abstract="PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq {\textasciitilde} 12.5\thinspace$\mu$g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 $\mu$g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.",
issn="1097-9867",
doi="10.3109/10837450903170772",
url="http://www.ncbi.nlm.nih.gov/pubmed/22716467",
language="eng"
}

%0 Journal Article
%T Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.
%A Adams, Monica L.
%A Rao, Venkatramana M.
%A Thakur, Ajit
%A Hussain, Munir A.
%J Pharmaceutical development and technology
%D 2010
%8 Jun
%V 15
%N 3
%@ 1097-9867
%G eng
%F Adams2010
%X PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq ~ 12.5??g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 ?g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.
%K Carboxylic Acids
%K Chemistry, Pharmaceutical
%K Colloids
%K Hydrogen-Ion Concentration
%K Micelles
%K Polyethylene Glycols
%K Polymers
%K Solubility
%K Surface-Active Agents
%K X-Ray Diffraction
%U http://dx.doi.org/10.3109/10837450903170772
%U http://www.ncbi.nlm.nih.gov/pubmed/22716467
%P 266-275

PT Journal
AU Adams, ML
   Rao, VM
   Thakur, A
   Hussain, MA
TI Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.
SO Pharmaceutical development and technology
JI Pharm Dev Technol
PD Jun
PY 2010
BP 266
EP 275
VL 15
IS 3
DI 10.3109/10837450903170772
LA eng
DE Carboxylic Acids; Chemistry, Pharmaceutical; Colloids; Hydrogen-Ion Concentration; Micelles; Polyethylene Glycols; Polymers; Solubility; Surface-Active Agents; X-Ray Diffraction
AB PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq ~ 12.5??g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 ?g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.
ER

PMID- 22716467
OWN - NLM
STAT- MEDLINE
DA  - 20120621
DCOM- 20131227
LR  - 20151119
IS  - 1097-9867 (Electronic)
IS  - 1083-7450 (Linking)
VI  - 15
IP  - 3
DP  - 2010 Jun
TI  - Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic 
      acid)s and effect on kinetic solubility under acidic conditions.
PG  - 266-75
LID - 10.3109/10837450903170772 [doi]
AB  - PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for
      solubilized oral formulations of weakly acidic compounds. Micelles of
      poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene
      glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence
      spectroscopy and dynamic light scattering revealed that both polymers assemble
      into nanoscopic structures (&lt; 200 nm) in acidic media and exhibit pH-sensitive
      colloidal phase behavior. Using a solvent evaporation technique, the block
      copolymers and corresponding PCA homopolymers were incorporated into
      PEG3350-based solid dispersions. The kinetic solubility profile of a BMS
      compound, BMS-A (Seq ~ 12.5 mug/mL at pH 1.1) in 0.1 N HCl was monitored as a
      function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in
      the absence of PEG-b-PCAs, a supersaturated level of ca. 400 mug/mL was
      maintained for variable lengths of time in the presence of PEG-b-PCAs. Although
      the kinetic solubility of BMS-A was also enhanced in the presence of the PCA
      homopolymers, the relative magnitude and duration of supersaturation as a
      function of polymer composition suggests that micellar solubilization, rather
      than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N
      HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic
      supersaturation necessary to minimize precipitation of compounds which have
      limited solubility in acidic milieu.
FAU - Adams, Monica L
AU  - Adams ML
AD  - Biopharmaceutics Research and Development, Bristol-Myers Squibb Company, New
      Brunswick, New Jersey 08903, USA. [email protected]
FAU - Rao, Venkatramana M
AU  - Rao VM
FAU - Thakur, Ajit
AU  - Thakur A
FAU - Hussain, Munir A
AU  - Hussain MA
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Pharm Dev Technol
JT  - Pharmaceutical development and technology
JID - 9610932
RN  - 0 (Carboxylic Acids)
RN  - 0 (Colloids)
RN  - 0 (Micelles)
RN  - 0 (Polymers)
RN  - 0 (Surface-Active Agents)
RN  - 30IQX730WE (Polyethylene Glycols)
SB  - IM
MH  - Carboxylic Acids/*chemistry/pharmacokinetics
MH  - Chemistry, Pharmaceutical/*methods
MH  - Colloids
MH  - Hydrogen-Ion Concentration
MH  - *Micelles
MH  - Polyethylene Glycols/*chemistry/pharmacokinetics
MH  - Polymers/chemistry/pharmacokinetics
MH  - Solubility
MH  - Surface-Active Agents/*chemistry/pharmacokinetics
MH  - X-Ray Diffraction/methods
EDAT- 2010/05/01 00:00
MHDA- 2013/12/29 06:00
CRDT- 2012/06/22 06:00
AID - 10.3109/10837450903170772 [doi]
PST - ppublish
SO  - Pharm Dev Technol. 2010 Jun;15(3):266-75. doi: 10.3109/10837450903170772.
TY  - JOUR
AU  - Adams, Monica L.
AU  - Rao, Venkatramana M.
AU  - Thakur, Ajit
AU  - Hussain, Munir A.
PY  - 2010/Jun/
TI  - Colloidal phase behavior of pH-responsive, amphiphilic PEGylated poly(carboxylic acid)s and effect on kinetic solubility under acidic conditions.
T2  - Pharm Dev Technol
JO  - Pharmaceutical development and technology
SP  - 266
EP  - 275
VL  - 15
IS  - 3
KW  - Carboxylic Acids
KW  - Chemistry, Pharmaceutical
KW  - Colloids
KW  - Hydrogen-Ion Concentration
KW  - Micelles
KW  - Polyethylene Glycols
KW  - Polymers
KW  - Solubility
KW  - Surface-Active Agents
KW  - X-Ray Diffraction
N2  - PEGylated poly(carboxylic acid)s, PEG-b-PCAs, were evaluated as additives for solubilized oral formulations of weakly acidic compounds. Micelles of poly(ethylene glycol)-block-poly(acrylic acid), PEG-b-PAA, and poly(ethylene glycol)-block-poly(methacrylic acid), PEG-b-PMAA, were prepared. Fluorescence spectroscopy and dynamic light scattering revealed that both polymers assemble into nanoscopic structures (< 200 nm) in acidic media and exhibit pH-sensitive colloidal phase behavior. Using a solvent evaporation technique, the block copolymers and corresponding PCA homopolymers were incorporated into PEG3350-based solid dispersions. The kinetic solubility profile of a BMS compound, BMS-A (Seq ~ 12.5??g/mL at pH 1.1) in 0.1 N HCl was monitored as a function of polymer composition. While BMS-A precipitated rapidly in 0.1 N HCl in the absence of PEG-b-PCAs, a supersaturated level of ca. 400 ?g/mL was maintained for variable lengths of time in the presence of PEG-b-PCAs. Although the kinetic solubility of BMS-A was also enhanced in the presence of the PCA homopolymers, the relative magnitude and duration of supersaturation as a function of polymer composition suggests that micellar solubilization, rather than specific interaction, contributes to enhanced solubility of BMS-A in 0.1 N HCl. Under acidic conditions, pH-responsive PEG-b-PCAs may offer the kinetic supersaturation necessary to minimize precipitation of compounds which have limited solubility in acidic milieu.
SN  - 1097-9867
UR  - http://dx.doi.org/10.3109/10837450903170772
UR  - http://www.ncbi.nlm.nih.gov/pubmed/22716467
ID  - Adams2010
ER  - 
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